Devasthale P, Wang Y, Wang W, Fevig J, Feng J, Wang A, Harrity T, Egan D, Morgan N, Cap M, Fura A, Klei HE, Kish K, Weigelt C, Sun L, Levesque P, Moulin F, Li YX, Zahler R, Kirby MS, Hamann LG (2013)
Optimization of Activity, Selectivity, and Liability Profiles in 5-Oxopyrrolopyridine DPP4 Inhibitors Leading to Clinical Candidate (Sa)-2-(3-(Aminomethyl)-4-(2,4-dichlorophenyl)-2-methyl-5-oxo-5H-pyrrolo[3,4-b]py ridin-6(7H)-yl)-N,N-dimethylacetamide (BMS-767778)
Journal of Medicinal Chemistry 56: 7343
Harstad EB, Rosenblum JS, Gorrell MD, Achanzar WE, Minimo L, Wu J, Rosini-Marthaler L, Gullo R, Ordway ND, Kirby MS, Chadwick KD, Cosma GN, Moyer CF (2013)
DPP8 and DPP9 expression in cynomolgus monkey and Sprague Dawley rat tissues
Regul Pept 186C: 26
Zhao G, Kwon C, Wang A, Robertson JG, Marcinkeviciene J, Parker RA, Kirby MS, Hamann LG (2013)
Substituted piperidinyl glycinyl 2-cyano-4,5-methano pyrrolidines as potent and stable dipeptidyl peptidase IV inhibitors
Bioorganic & Medicinal Chemistry Lett 23: 1622
Wang A, Dorso C, Kopcho L, Locke G, Langish R, Harstad E, Shipkova P, Marcinkeviciene J, Hamann L, Kirby MS (2012)
Potency, selectivity and prolonged binding of saxagliptin to DPP4: maintenance of DPP4 inhibition by saxagliptin in vitro and ex vivo when compared to a rapidly-dissociating DPP4 inhibitor
BMC Pharmacol 12: 2
Wang W, Devasthale P, Wang A, Harrity T, Egan D, Morgan N, Cap M, Fura A, Klei HE, Kish K, Weigelt C, Sun L, Levesque P, Li YX, Zahler R, Kirby MS, Hamann LG (2011)
7-Oxopyrrolopyridine-derived DPP4 inhibitors-mitigation of CYP and hERG liabilities via introduction of polar functionalities in the active site
Bioorganic & Medicinal Chemistry Lett 21: 6646
Brigance RP, Meng W, Fura A, Harrity T, Wang A, Zahler R, Kirby MS, Hamann LG (2010)
Synthesis and SAR of azolopyrimidines as potent and selective dipeptidyl peptidase-4 (DPP4) inhibitors for type 2 diabetes
Bioorganic & Medicinal Chemistry Lett 20: 4395
Meng W, Brigance RP, Chao HJ, Fura A, Harrity T, Marcinkeviciene J, O'Connor SP, Tamura JK, Xie D, Zhang Y, Klei HE, Kish K, Weigelt CA, Turdi H, Wang A, Zahler R, Kirby MS, Hamann LG (2010)
Discovery of 6-(Aminomethyl)-5-(2,4-dichlorophenyl)-7-methylimidazo[1,2-a]pyrimidine-2-carboxa mides as Potent, Selective Dipeptidyl Peptidase-4 (DPP4) Inhibitors
Journal of Medicinal Chemistry 53: 5620
O'Connor SP, Wang Y, Simpkins LM, Brigance RP, Meng W, Wang A, Kirby MS, Weigelt CA, Hamann LG (2010)
Synthesis, SAR, and atropisomerism of imidazolopyrimidine DPP4 inhibitors
Bioorganic & Medicinal Chemistry Lett 20: 6273
Metzler WJ, Yanchunas J, Weigelt C, Kish K, Klei HE, Xie D, Zhang Y, Corbett M, Tamura JK, He B, Hamann LG, Kirby MS, Marcinkeviciene J (2008)
Involvement of DPP-IV catalytic residues in enzyme-saxagliptin complex formation
Protein Science 17: 240
Simpkins LM, Bolton S, Pi Z, Sutton JC, Kwon C, Zhao G, Magnin DR, Augeri DJ, Gungor T, Rotella DP, Sun Z, Liu Y, Slusarchyk WS, Marcinkeviciene J, Robertson JG, Wang A, Robl JA, Atwal KS, Zahler RL, Parker RA, Kirby MS, Hamann LG (2007)
Potent non-nitrile dipeptidic dipeptidyl peptidase IV inhibitors
Bioorganic & Medicinal Chemistry Lett 17: 6476
Magnin DR, Taunk PC, Robertson JG, Wang A, Marcinkeviciene J, Kirby MS, Hamann LG (2006)
Seco-prolinenitrile inhibitors of dipeptidyl peptidase IV define minimal pharmacophore requirements at P1
Bioorganic & Medicinal Chemistry Lett 16: 1731
Augeri DJ, Robl JA, Betebenner DA, Magnin DR, Khanna A, Robertson JG, Wang A, Simpkins LM, Taunk P, Huang Q, Han SP, Abboa-Offei B, Cap M, Xin L, Tao L, Tozzo E, Welzel GE, Egan DM, Marcinkeviciene J, Chang SY, Biller SA, Kirby MS, Parker RA, Hamann LG (2005)
Discovery and preclinical profile of Saxagliptin (BMS-477118): a highly potent, long-acting, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes
Journal of Medicinal Chemistry 48: 5025
Kopcho LM, Kim YB, Wang A, Liu MA, Kirby MS, Marcinkeviciene J (2005)
Probing prime substrate binding sites of human dipeptidyl peptidase-IV using competitive substrate approach
Archives of Biochemistry & Biophysics 436: 367
Zhao G, Taunk PC, Magnin DR, Simpkins LM, Robl JA, Wang A, Robertson JG, Marcinkeviciene J, Sitkoff DF, Parker RA, Kirby MS, Hamann LG (2005)
Diprolyl nitriles as potent dipeptidyl peptidase IV inhibitors
Bioorganic & Medicinal Chemistry Lett 15: 3992